Compositions and methods for minimizing and/or reducing the appearance of defects around eyes

ABSTRACT

The invention relates to compositions comprising at least one xanthine compound, preferably further comprising at least one agent which acts on capillary circulation and/or at least one natural moisturizing agent, which can be used to treat, or to reduce and/or minimize the appearance of, defects such as dark circles, bags and/or puffiness around eyes.

FIELD OF THE INVENTION

The present invention relates to compositions such as cosmetic ordermatologic compositions comprising at least one xanthine compound.Preferably, the compositions further comprise at least one agent whichacts on capillary circulation and/or at least one natural moisturizingagent. Such compositions can be used, in particular, to treat or toreduce and/or minimize the appearance of defects such as dark circles,bags and/or puffiness around eyes.

DISCUSSION OF THE BACKGROUND

The eye contour (area around the eyes) has a very important aestheticrole since it immediately reflects fatigue, humor and age.

The eye contour, owing to its structure and its high innervation, is ananatomical site that is particularly sensitive to environmental factors(UV rays, pollution, tobacco, etc.) and physiological factors (fatigue,stress, etc.).

In humans, the eyes blink a thousand times per day, and the epidermiswhich surrounds them is very thin and not very well irrigated—to allowsignificant mobility, the skin around the eyes is extremely thin (on theorder of 0.33 to 0.36 mm, i.e., 3 to 5 times thinner than the rest ofthe skin of the face). Thus, it is easily dehydrated and vulnerable toexternal aggressions, meaning that such skin requires particular care.

The skin around the eyes can also reflect one's lifestyle to a certainextent: heat, stress, tobacco, UV rays, and facial expressions can leadto multiple variations of this skin throughout the day which involvevascularization, hydration and turgescence of skin tissues and can helpexplain the principal changes observed: swelling, dark circles,puffiness, etc.

Moreover, the skin of the eye contour is very reactive due to itsrichness in inflammatory cells (mast cells), meaning that such skin canbe sensitive or intolerant leading, perhaps, to allergic reactions.

Furthermore, the skin of the eye contour can be particularly sensitiveto solar radiation. Excessive exposure without protection can lead toredness, sensitivity, or even swelling via microcirculation disorders.

Dark circles and swelling of the eye contour can have a vascular orhereditary origin. Surface vascularization is barely visible in suchskin, since the capillaries have a low flow rate, but the vessels of thesubcutaneous layers constitute a large vascular reserve which may varythroughout the day. Dark circles generally correspond to a transitory orpermanent vascular congestion which results in hyperpigmentation of theskin, and are typically accentuated by at least some of the factorsdiscussed above.

The formation of dark circles often occurs as a result of slowing bloodmicrocirculation, especially at night, which leads to an accumulation ofblood pigments in the conjunctive tissue. Furthermore, the lymphaticsystem, also slowed during the night, leads to swelling of this skin.Such swelling, associated with age-related slackening of the tissues,can help cause the formation of bags.

Defects around eyes such as dark circles and swelling have always beenconsidered to be unattractive, and it has always been a goal to maskthem or even eliminate them.

There remains a need for compositions which can reduce and/or minimizethe appearance of defects of the contour of the eyes, in particularbags, dark circles and/or puffiness, and for effective methods ofreducing and/or minimizing the appearance of such defects in skin aroundeyes.

SUMMARY OF THE INVENTION

The present invention relates to compositions comprising at least onexanthine compound. Preferably, the compositions further comprise atleast one agent which acts on capillary circulation and/or at least onenatural moisturizing agent.

The present invention also relates to a roll-on applicator comprising acomposition comprising at least one xanthine compound. Preferably, thecompositions further comprise at least one agent which acts on capillarycirculation and/or at least one natural moisturizing agent.

The present invention further relates to methods for treating defectsaround eyes such as, for example, dark circles, bags and/or puffiness,comprising topically applying to the skin around eyes a compositioncomprising at least one xanthine compound. Preferably, the compositionsfurther comprise at least one agent which acts on capillary circulationand/or at least one natural moisturizing agent. Also preferably,application of the composition to the skin around eyes occurs withoutcontacting the composition with human hands and/or fingers prior toapplication.

The present invention further relates to methods for reducing and/orminimizing the appearance of defects around eyes such as, for example,dark circles, bags and/or puffiness, comprising topically applying tothe skin around eyes a composition comprising at least one xanthinecompound. Preferably, the compositions further comprise at least oneagent which acts on capillary circulation and/or at least one naturalmoisturizing agent. Also preferably, application of the composition tothe skin around eyes occurs without contacting the composition withhuman hands and/or fingers prior to application.

It is to be understood that both the foregoing general description andthe following detailed description are exemplary and explanatory only,and are not restrictive of the invention.

DETAILED DESCRIPTION OF THE INVENTION

As used herein, the expression “at least one” means one or more and thusincludes individual components as well as mixtures/combinations.

Other than in the operating examples, or where otherwise indicated, allnumbers expressing quantities of ingredients and/or reaction conditionsare to be understood as being modified in all instances by the term“about,” meaning within 10% to 15% of the indicated number.

“Contour of the eye” or “around the eye” means an area located aroundthe eye, in particular underneath the eye and the upper eyelid.

“Dark Circle” refers to an area of discoloration in at least a portionof the contour of the eye.

“Puffiness” and “bags” are generally equivalent and mean swelling in atleast a portion of the contour of the eye.

“Substituted” as used herein, means comprising at least one substituent.Non-limiting examples of substituents include atoms, such as oxygenatoms and nitrogen atoms, as well as functional groups, such as hydroxylgroups, ether groups, alkoxy groups, acyloxyalky groups, oxyalkylenegroups, polyoxyalkylene groups, carboxylic acid groups, amine groups,acylamino groups, amide groups, halogen containing groups, ester groups,thiol groups, sulphonate groups, thiosulphate groups, siloxane groups,and polysiloxane groups. The substituent(s) may be further substituted.

The compositions and methods of the present invention can comprise,consist of, or consist essentially of the essential elements andlimitations of the invention described herein, as well as any additionalor optional ingredients, components, or limitations described herein orotherwise useful.

Compositions Comprising at Least One Xanthine Compound

According to the present invention, compositions comprising at least onexanthine compound are provided. Such xanthine compounds can either bethe xanthine compound per se or an extract comprising the xanthinecompound such as, for example, a natural extract.

Suitable xanthine compounds include, but are not limited to, xanthinecompounds per se such as theophylline, caffeine, theobromine,acefylline, xanthinol nicotinate, diniprophylline, diprophylline,etamiphylline and its derivatives, etophylline, proxyphylline,pentophylline, propentophylline, pyridophylline, bamiphylline, andmixtures thereof. Of these, caffeine, theophylline, theobromine, andacefylline are preferred, with caffeine being particularly preferred. Anexample of a commercially available xanthine compound suitable for usein the invention compositions is caffeine sold by the company BASF(Caffeine Anhydrous Powder).

Suitable xanthine compound containing extracts include, but are notlimited to, extracts such as plant extracts such as extracts of tea, ofcoffee, of guarana, of Paraguay tea, of cola, and mixtures thereof.

In accordance with preferred embodiments, the xanthine compound ispreferably present in the composition in an amount of from 0.01% to 10%by weight, preferably from 0.1% to 7% by weight, of the total weight ofthe composition, including all ranges and subranges therebetween. Whenan extract containing a xanthine compound is present in the composition,these ranges refer to the amount of xanthine compound per se present,not the amount of extract present.

According to particularly preferred embodiments of the presentapplication, compositions further comprising at least one agent whichacts on capillary circulation are provided. Such agents can either bethe agent per se or an extract comprising the agent such as, forexample, a natural extract.

Suitable agents which act on capillary circulation include, but are notlimited to, vasoprotectors and vasodilators, specific examples of whichinclude, for example, flavonoids, extracts of Ginkgo biloba,ruscogenins, esculosides, rutin, escin extracted from commonhorsechestnut, nicotinates, hesperidine methyl chalcone,butcher's-broom, essential oils of lavender or of rosemary, extracts ofAmmi Visnaga, and mixtures thereof. According to preferred embodiments,the invention compositions comprise escin. Escin is a mixture oftriterpenic pentacyclic acylated saponins obtained from the extractionof the seeds of Horse chestnut (Aesculus Hippocastanum L.). An exampleof commercially available escin is that sold by the company Indenas.p.a. (Escin Free Acid).

In accordance with preferred embodiments, the agent which acts oncapillary circulation, if present, is preferably present in thecomposition in an amount of from 0.01% to 10% by weight, preferably from0.05% to 5% by weight, of the total weight of the composition, includingall ranges and subranges therebetween. When an extract containing anagent which acts on capillary circulation is present in the composition,these ranges refer to the amount of agent per se present, not the amountof extract present.

According to particularly preferred embodiments of the presentapplication, compositions further comprising at least one naturalmoisturizing agent are provided. A “natural moisturizer” is a naturallyoccurring biological compound which helps maintain moisturization of thestratum corneum and/or which increases water content of the stratumcorneum.

Suitable natural moisturizers include, but are not limited to,lecithins, glycosphingolipids, phospholipids, cholesterol and itsderivatives, phytosterols (stigmasterol, β-sitosterol or campesterol),essential fatty acids, hyaluronic acid and its derivatives, ectoin andits derivatives, chitosan, sugars (for example, rhamnose, threalose,glucose), adenosine and its derivatives, ceramides, c-glycosides (forexample, modulators of proteoglycans and/or glycoaminoglycans such asthose sold under the Pro-xylane® name), and mixtures thereof.

According to particularly preferred embodiments of the presentinvention, hyaluronic acid or a derivative is present in thecomposition. Hyaluronic acid belongs to the glycosaminoglycan (GAG)family. GAGs are linear chains composed of a repetition of a basediholoside always containing a hexosamine (glucosamine or galactosamine)and another monosaccharide (glucuronic acid, iduronic acid orgalactose). Glucosamine is either N-sulphated or N-acetylated. On theother hand, galactosamine is always N-acetylated. In addition, there maybe sulphates O-bonded to the hexosamine, uronic acid and galactose.

Hyaluronic acid or hyaluronan (HA) is the principal GAG of the dermis,the latter containing half the organism's HA. It is a polysaccharide ofdisaccharides that are themselves composed of D-glucuronic acid and ofN-acetylglucosamine, linked to one another via alternating beta-1,4 andbeta-1,3 glycosidic bonds.

According to preferred embodiments, the composition according to thepresent invention contains hyaluronic acid and/or one of its salts.Suitable hyaluronic acid salts include, but are not limited to,potassium hyaluronate and sodium hyaluronate, with sodium hyaluronatebeing particularly preferred. For example, sodium hyaluronate with amolecular weight of 1,100,000 daltons, sold by the company SOLIANCEunder the name CRISTALHYAL®, may be used.

In accordance with preferred embodiments, the natural moisturizingagent, if present, is preferably present in the composition in an amountof from 0.01% to 5% by weight, preferably from 0.01% to 3% by weight,preferably from 0.01 to 1% by weight, of the total weight of thecomposition, including all ranges and subranges therebetween. When aproduct containing a natural moisturizing agent is present in thecomposition, these ranges refer to the amount of agent per se present,not the amount of product present.

In accordance with the present invention, the composition comprising atleast one xanthine compound, preferably further comprising at least oneagent which acts on capillary circulation and/or at least one naturalmoisturizing agent, comprises active agent(s) present, alone or in anycombination thereof, in an amount sufficient to treat defects of the eyecontour, particularly bags, puffiness and/or dark circles, or to reduceand/or minimize the appearance of defects of the eye contour,particularly bags, puffiness and/or dark circles. Such effects may bemeasured by simple visual observation or by comparative image analysis.

The composition of the invention can further optionally comprise anyadditive usually used in the field under consideration. For example,vitamins such as vitamin A, vitamin B, vitamin C, vitamin D, etc., andderivatives thereof such as, for example, retinol, retinyl palmitate,panthenol and in particular D-panthenol, ascorbyl palmitate, etc., oils,water, pigments, solvents such as polyols and in particular butyleneglycol and/or glycerine, film forming agents, dispersants, antioxidants,sunscreens, preserving agents, fragrances, fillers, neutralizing agents,surfactants, emulsifiers, hydrophilic or lipophilic gelling agents,hydrophilic or lipophilic additives, screening agents, ph adjusters,colorants, sequestrants, chelating agents, odor absorbers and mixturesthereof can be added. A non-exhaustive listing of such ingredients canbe found in U.S. patent application publication no. 2004/0170586, theentire contents of which is hereby incorporated by reference. Furtherexamples of suitable additional components can be found in the otherreferences which have been incorporated by reference in thisapplication. Still further examples of such additional ingredients maybe found in the International Cosmetic Ingredient Dictionary andHandbook (9^(th) ed. 2002). Other ingredients such as Guanosine andHydroxyproline, may also be added.

A person skilled in the art will take care to select the optionaladditional additives and/or the amount thereof such that theadvantageous properties of the composition according to the inventionare not, or are not substantially, adversely affected by the envisagedaddition.

These substances may be selected variously by the person skilled in theart in order to prepare a composition which has the desired properties,for example, consistency or texture.

These additives may be present in the composition in a proportion from0% to 99% (such as from 0.01% to 90%) relative to the total weight ofthe composition and further such as from 0.1% to 50% (if present),including all ranges and subranges therebetween.

Needless to say, the composition of the invention should be cosmeticallyor dermatologically acceptable, i.e., it should contain a non-toxicphysiologically acceptable medium and should be able to be applied tothe contour of the eye of human beings. The composition may be in anygalenic form normally employed in the cosmetic and dermatological fieldswhich is suitable for topical administration onto skin. Aqueouscompositions are preferred, with aqueous compositions in the form of agel being particularly preferred. If the composition is in the form of agel, the composition preferably comprises at least one gelling agentwhich may be any gelling agent suitable for use in the cosmetic area.For example, suitable gelling agents include, but are not limited to,carboxyvinyl polymers (carbomer), acrylic copolymers such asacrylate/alkyl acrylate copolymers, polyacrylamides optionally in theform of copolymers in an inverse emulsion, such as the products sold,respectively, by CLARIANT under the trade name HOSTACERIN AMPS and bySEPPIC under the trade name SEPIGEL 305, polysaccharides, such asxanthan gum. In such gel compositions, the water content is preferablyhigher than 50% of the total weight of the composition.

Methods of Addressing Defects Around the Eyes Using the Composition ofthe Present Invention

According to preferred embodiments of the present invention, methods oftreating defect(s) of the contour of the eye comprising applying acomposition of the present invention to the contour of the eye in anamount sufficient to treat the defect(s) are provided.

According to other preferred embodiments, methods of reducing and/orminimizing the appearance of defect(s) of the contour of the eyecomprising applying a composition of the present invention to thecontour of the eye in an amount sufficient to reduce and/or minimize theappearance of the defect(s) are provided.

In accordance with preferred embodiments of the preceding methods, acomposition of the present invention comprising at least one xanthinecompound, preferably further comprising at least one agent which acts oncapillary circulation and/or at least one natural moisturizing agent,are applied topically to the contour of the eye of a person in need ofthe desired treatment, reduction and/or minimization in an amountsufficient to achieve the desired result. The compositions may beapplied to the desired area as needed, preferably once or twice daily.

Preferably, application begins at the inner corner of the eye (proximateto the nose), and continues along the contour toward the outer corner ofthe eye. However, the reverse direction of application can also occur.

According to particularly preferred embodiments, application of thecomposition to the skin around eyes occurs without contacting thecomposition with human hands and/or fingers prior to application. Thatis, application occurs via an applicator which enables the user to avoidcontacting the composition prior to application. Such application,without contact with human skin prior to application, can improveefficacy of the composition. Although not wishing to be bound by anyparticular theory, it is believed that such pre-application contactraises the temperature of the composition prior to application, whichcan have the effect of negatively affecting the composition's efficacy.

Suitable application methods (without contacting the user's hands orfingers) include but are not limited to application using a roll-ondispenser or applicator (for example, the type of dispenser orapplicator used to apply roll-on deodorants) and application using anapplicator pad or wipe.

According to particularly preferred embodiments of the presentinvention, a roll-on dispenser or applicator is used to apply thecomposition of the present invention to the contour of the eye. Inaccordance with such preferred embodiments, the roll-on dispenser orapplicator comprises a reservoir having a base and, opposite the base,an opening. The reservoir can be made of various materials such as, forexample, glass or a plastic like polypropylene, polyethyleneterephthalate (PET), acrylobutadiene styrene (ABS), or polyethylene, andcan be of any shape. The reservoir contains the composition of thepresent invention.

Mounted in the opening is a rotatable ball which, for example, can beassembled directly in the reservoir or through a special insert (ballhousing) depending on the size and design of the reservoir. Typically,the rotatable ball is hollow. The rotatable ball can be of any suitablematerial such as, for example, glass, plastic (such as those mentionedabove in connection with the reservoir) or metal. Metals such as, forexample, stainless steel, aluminum, and silver may be used, withstainless steel being preferred. The diameter of the ball will, ofcourse, vary depending on the size of the opening in the reservoir.Preferably, the rotatable ball does not substantially change thetemperature of the composition of the present application duringapplication. During application, the composition of the presentinvention is applied to the skin of the contour of the eye through therotating or rolling action of the rotatable ball.

Examples of suitable roll-on dispensers include those described in U.S.Des. Pat. No. 402,550, and U.S. Pat. Nos. 6,511,657, 6,132,126,4,030,844, 4,021,125, 4,033,700, and 5,553,957, all of which areincorporated by reference herein including their drawings to the extentthey describe roll-on dispensers.

The present invention also relates to a roll-on applicator as describedabove comprising a composition comprising at least one xanthinecompound. Preferably, the compositions further comprise at least oneagent which acts on capillary circulation and/or at least one naturalmoisturizing agent.

Unless otherwise indicated, all numbers expressing quantities ofingredients, reaction conditions, and so forth used in the specificationand claims are to be understood as being modified in all instances bythe term “about.” Accordingly, unless indicated to the contrary, thenumerical parameters set forth in the following specification andattached claims are approximations that may vary depending upon thedesired properties sought to be obtained by the present invention.

Notwithstanding that the numerical ranges and parameters setting forththe broad scope of the invention are approximations, the numericalvalues set forth in the specific examples are reported as precisely aspossible. Any numerical value, however, inherently contain certainerrors necessarily resulting from the standard deviation found in theirrespective measurements. The following examples are intended toillustrate the invention without limiting the scope as a result. Thepercentages are given on a weight basis.

EXAMPLES Example 1 Composition

BUTYLENE GLYCOL 5 XANTHAN GUM 0.4 CAPRYLYL GLYCOL 0.3 GUANOSINE 0.01DISODIUM EDTA 0.2 BIOSACCHARIDE GUM-1 5 POLYACRYLAMIDE (and) C13-14 0.4ISOPARAFFIN (and) LAURETH-7 HYDROXYPROLINE 0.3 GLYCERIN 3 CAFFEINE 0.5ESCIN 0.05 WATER 83.87 PANTHENOL 0.5 SODIUM HYALURONATE 0.02PRESERVATIVE AGENTS 0.45 Total: 100

indicates data missing or illegible when filed

Example 2 Application of the Composition of Example 1 to the Contour ofthe Eye—Moisturizing Effect

The composition of example 1 was placed into a roll-on dispenser. 24subjects applied the composition of example 1 to the contour of theireyes using the dispenser a single time. The skin of the subjectsthus-treated 4 hours after application as well as 8 hours afterapplication was compared to the skin prior to treatment. The subjects'skin was evaluated using a corneometer which estimated the water contentin stratum corneum of the skin from electric capacitance—the higher thewater content, the higher the conductance or electric capacitance ofskin surface. Via this method, the water content of the stratum corneumwas quantitatively determined. The results are set forth below.

Improvement vs TO T4 hours +21% T8 hours +15%

The composition of example 1 when applied to skin using a roll-ondispenser had a significant moisturizing effect 4 hours afterapplication as well as 8 hours after application as compared tonon-treated skin.

Example 3 Application of the Composition of Example 1 to the Contour ofthe Eye—Effect on Bags and Dark Circles

The composition of example 1 was placed into a roll-on dispenser. 151subjects applied the composition of example 1 to the contour of theireyes using the dispenser, twice a day, for four weeks. 50 of thesesubjects were subjected to clinical grading; 101 subjects were subjectto self-assessment. All of the subjects had bags and/or dark circles inthe contour of the eyes. All skin types were represented in the group of151. The results are set forth below.

Clinical Grading—Efficacy on Dark Circles and Bags

Dermatologists evaluated the bags and dark circles of 50 subjects anddetermined:

Improvement after 4 weeks Bags −11% Dark circles −12%

The composition of example 1 when applied to skin using a roll-ondispenser had a significant effect on both bags and dark circles after 4weeks of use.

Self Assessment—Perceived Efficacy

101 subjects were provided questionnaires concerning the efficacy of thecomposition of example 1. Their answers are set forth below.

T Immediate T 4 weeks Skin looks more hydrated 86% 93% Skin feels morecomfortable 88% 89% Skin looks more uniform 63% 85% Upper eyelids lookless puffy — 77% The product brings freshness upon application 94% Theproduct does not leave skin sticky — 92% The product does not leave skingreasy — 100%  The product does not leave skin shiny — 95%

Example 4 Comparison of Application Methods

The composition of example 1 was placed into a roll-on dispenser forapplication. 23 subjects, women ranging from 21 to 50 years old, appliedthe composition of example 1 to the contour of their eyes a single time.Application to the contour of the eye on one side of the face occurredusing a finger. Application to the contour of the eye on the other sideof the face occurred using the roll-on dispenser. The sides wererandomized among the women. The skin of the subjects thus-treated wasevaluated by IR camera. The results were as follows.

The composition applied with the fingers yielded a fresh effect in 1min., 41 sec. (corresponding to a decrease of initial temperature (−2.6°C.)).

In contrast, the composition applied using a roll-on dispenser yielded afresh effect in 59 seconds (corresponding to a decrease of initialtemperature (−2.1° C.)). This time differential in achieving thetemperature decrease (fresh effect) was statistically significant

Application using a roll-on dispenser permitted obtaining the fresheffect more quickly.

1. A roll-on applicator comprising a reservoir and a rotatableapplication surface capable of being in fluid communication with thereservoir wherein the reservoir contains a composition comprising atleast one xanthine compound, at least one agent which acts on capillarycirculation, and at least one natural moisturizing agent.
 2. A roll-onapplicator according to claim 1, wherein the rotatable applicationsurface is an outer surface of a sphere made from metal, glass, plasticor ceramic.
 3. The roll-on applicator of claim 1, wherein thecomposition further comprises a vitamin compound.
 4. The roll-onapplicator of claim 3, wherein the vitamin compound is panthenol.
 5. Theroll-on applicator of claim 1, wherein the xanthine compound iscaffeine.
 6. The roll-on applicator of claim 5, wherein the at least oneagent which acts on capillary circulation is escin.
 7. The roll-onapplicator of claim 6, wherein the natural moisturizing agent is sodiumhyaluronate.
 8. The roll-on applicator of claim 7, wherein thecomposition further comprises a vitamin compound.
 9. The roll-onapplicator of claim 8, wherein the vitamin compound is panthenol. 10.The roll-on applicator of claim 1, wherein the composition furthercomprises guanosine and/or hydroxyproline.
 11. A method of reducing orminimizing dark circles, bags or puffiness on the contours of eyes of aperson in need thereof comprising applying a composition comprising atleast one xanthine compound, at least one agent which acts on capillarycirculation, and at least one natural moisturizing agent to the contoursof eyes using a roll-on applicator in an amount sufficient to minimizeor reduce the bags, dark circles or puffiness.
 12. The method of claim11, wherein the composition further comprises a vitamin compound. 13.The method of claim 12, wherein the vitamin compound is panthenol. 14.The method of claim 11, wherein the xanthine compound is caffeine. 15.The method of claim 14, wherein the at least one agent which acts oncapillary circulation is escin.
 16. The method of claim 15, wherein thenatural moisturizing agent is sodium hyaluronate.
 17. The method ofclaim 16, wherein the composition further comprises a vitamin compound.18. The method of claim 17, wherein the vitamin compound is panthenol.19. A roll-on applicator comprising a reservoir and a rotatableapplication surface capable of being in fluid communication with thereservoir wherein the reservoir contains a composition comprisingcaffeine, escin and sodium hyaluronate.